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3 classes of Anticoagulants
- Anticoagulants
- Fibrinolytics
- Antiplatelets
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6 Anticoagulants
- Heparins: aka HMWH; activates antithrombinIII
- LMWH/Enoxoparin: specific inhibition of factorXa
- Lepirudin: binds soluble and bound thrombin
- Warfarin/coumadin: inhibits vitK epoxide reductase
- Drotrecogin-α: recomb human Activated Protein C; cleaves fVa,VIIa
- Dabigatran etexilate: novel oral anticoag; stroke; direct competitive inhibition of thrombin
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4 Fibrinolytics (anticoag)
- Streptokinase: activates plasmin; not available in US
- Alteplase: converts fibrin-bound plasminogen to plasmin
- Reteplase: same as alteplase, also binds fibrin
- Tenecteplase: same as reteplase
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3 antiplatelet drugs (anticoag)
- Aspirin: blocks thromboxane A2 synth via irreversible COX inhibition
- Clopidogrel: blocks platelet ADP receptors, preventing fibrinogen-based activation
- Abciximab: inhibiting MAB against IIb/IIIa, preventing activation
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6 drugs that facilitate clotting
- VitK: essential clotting cofactor; coumarin tox
- Factor VIII: clotting factor replacement
- Factor IX: clotting factor replacement
- Desmopressin: increases plasma [clotting factors]
- Aminocaproic acid: not on US market
- Protamine sulphate: binds heparin, blocks anticoag effect
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9 drugs against Plasmodial infection (malaria)
- Proguanil: prophylaxis/suppression of P. falciparum, acute suppression of P. vivax
- Primaquine: Gametocytocidal for all Plasmodium; hypnozoitocidal for P. vivax and ovale
- Chloroquine: schizonticidal for all sensitive Plasmodium spp
- Quinine: same as chloroquine
- Quinidine: Tx of non-immune persons and multidrug resistant falciparum,
- Mefloquine: prophylaxis for multidrug resistant falciparum
- Doxycycline: same as mefloquine
- Artemisinin: Tx of non-immune persons for falciparum
- all of the above have same MoA - buildup of free radicals in microbe
- Antifolates: Pyrimethamine+sulfadioxine; inhibits parasite dihydrofolate reductase
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8 drugs against other protozoal (non-Plasmodial) infections
- Metronidazole: Entamoeba hystolytica, Giardia lamblia, and Trichomonas vaginalis; only approved nitroimidazole in US; prodrug that acts as e- sink for parasite
- Diloxanide furoate: given with metronidazole
- Tinidazole: same as metronidazole
- Nifurtimox: Trypanosoma cruzi; free radical production
- Stilbogluconate Na: Leishmania donovani;
- Paromomycin: same as stilbo; also Cryptosporidium
- Suramin: Trypanosoma cruzi
- Tetracyclines: Balantidium coli
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4 classes of Immunosuppressive drugs
- Toxic to all dividing cells
- Toxic to lymphocytes
- Toxic to a subpopulation of immune cells
- Molecular targeted MABs against cytokines w/ toxic outcomes
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1 Pan-Cytotoxic immunosuppressive\
- Azathioprine: de novo purine synth, acts in S phase; also antimalignant/arthritic
- Mercaptopurine: downstream metabolite of azathioprine, same MoA
- Allopurinol: given concomittantly; can increase mercaptopurine tox
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6 Lymphotoxic immunosuppressives
- ALG: antilymphocytic globulin; activates complement against T-cells
- IV Ig: pooled Ig's from healthy donors
- Rho (D) Ig: anti-Rh IgG to prevent newborn hemolysis
- Muromonab-CD3: blocks T-cell antigen recognition; acute renal allograft rejection
- Asparaginase: cleaves Asn to Asp, robbing from AA pool; anticancer
- Glucocorticoids: genetic immunosuppression
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4 immunosuppressives toxic to subpopulations of immune cells
- Cyclosporine: binds cyclophillin-A (blocks calcineurin), suppresses IL-2
- Tacrolimus: 10-100x as potent as cyclosporine; binds FKBP12 (blocks calcineurin) to suppress IL-2
- Sirolimus: inhibits mTOR, stopping G1->S progression
- Mycophenylate mofetil: inhibits IMP dehydrogenase (de novo guanine synth), selective for B/T-cells
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4 molecular-targeting immunosuppressives
- Etanercept: TNF-α receptor
- Infliximab: TNF-α antibody
- Abciximab: non-specific MAB (IIb/IIIa, others)
- Daclizumab: IL-2 receptor antibody, prevents CD4 activation
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2 main Immunostimulant "classes"
- Bacillus Calmette-Guerin (BCG): non-specific immunostimulant
- Recombinant Cytokines
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3 classes of immunostimulant Cytokines
- Interferons
- Interleukins
- Colony-stimulating factors
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3 immunostimulant Interferons
- Interferon-α: upreg MHC-I, downreg MHC-II; hairy cell leuk, hepB/C
- Interferon-β-1a/1b: multiple sclerosis
- Interferon-γ: phagocytes; chronic granulomatosis disease
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2 immunostimulant Interleukins
- Aldesleukin: IL-2; metastatic renal carcinoma, melanoma
- Oprelvekin: IL-11; stimulates platelet formation
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4 immunostimulant Colony-Stimulating Factors
- Filgrastim: G-CSF, stimulates bone marrow recovery during chemo and PMN proliferation
- Sargramostim: GM-CSF, non-lineage specific; myeloid recovery after chemo
- Epoetin-α: recombinant EPO; given with cisplatin
- Thrombopoietin: either molecule or fusion protein of GM-CSF and IL-3
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7 major classes of Antimalignant drugs
- Antimetabolites: rob cells of products necessary for division; e.g. methotrexate, blocks THF synth
- Alkylating Agents: x-links DNA to prevent transcription/translation
- Cytotoxic antibiotics: Cell-Cycle NonSpecific (CCNS), generally break or otherwise interfere with DNA
- Natural Products: depending, either topoisomerase or tubule activity
- Hormones: depends on cancer
- Immunosuppresants: name says it all
- Others: interferon, ILs, antibodies, platinums
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2*, 2** Antimetabolite antineoplastics
- *Methotrexate: blocks DiHydroFolate Reductase
- *5-Fluorouracil: incorporated into RNA, rendering it useless
- **Capecitabine: prodrug of 5-FU, non-responsive colorectal and breast
- **Cytarabine: blocks DNA elong; AML drug
- Azathioprine/mercaptopurine - anti-PRPP stuff
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2*, 2** Alkylating antineoplastics
- *Cyclophosphamide: prodrug -> nitrogen mustard, acrolein that x-links DNA; SIADH
- *Cisplatin: directly x-links DNA
- **Carmustine: CNS tox, CNS cancers
- **Temozolamide: success against malignant gliomas
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2*, 2** Cytotoxic Antibiotic antineoplastics
- *Doxorubicin: topoII poison; free radical formation
- *Bleomycin: Cu-chelating peptides; fragments DNA
- **Daunorubicin: leukemia
- **Dactinomycin: suppress hematopoiesis to pancytopenia
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3*, 2** Natural antineoplastics
- *Vincristine, *Vinblastine: alkaloids, bind tubulin preventing microtubule assembly
- **Etoposide: stabilizes topoII-DNA complex, breaking dsDNA
- **Topotecan: topoI inhibitor
- *Paclitaxel/docetaxel: taxanes; inhibit microtubule disassembly
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3*, 4**, Hormone/Antihormone antineoplastics
- *Tamoxifen: anti-estrogen
- *Prednisone: replacement
- *Prednisolone: replacement
- **Anastrazole: aromatase inhibitor
- **Finasteride: DHT inhibitor (5-α reductase)
- **Flutamide: antiandrogen
- **Leuprolide: GRH; inhibits LH/FSH
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6 Immunosuppressant antineoplastics
azathioprine, prednisolone, antilymphocytic globulin, cyclosporine, tacrolimus, mycophenolate
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1*, 5** "other" antineoplastics
- *Cisplatin: binds DNA, nephrotox
- **Asparaginase: prevents Asn synth; ALL
- **Rituximab: chimeric anti-CD20, facilitating complement; add w/ CHOPS
- **Trastuzumab: tx of HER2 breast cancer
- **Hydroxyurea: inhibits ribonucleotide reductase (no ribo -> deoxy)
- **Imatinib mesylate: inhibits BCR-ABL tyr-kin in CML
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5 classes of Antiretroviral (HIV) Drugs
- NRTI: nucleotide reverse-transcriptase inhibitors (ZELDAS)
- NNRTI: non-nucleotide reverse transcriptase inhibitors (DEN)
- PI: protease inhibitors (NEVER = navir)
- Integrase Inhibitors: prevent viral genome from entering host genome (STOP = ralt, Spanish for stop)
- Entry Inhibitors: block viral entry (SMOKING = fumar, enfu and marav)
- Zeldas Den Never Stop Smoking!
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6 NRTIs
- Zidovudine: front-runner in control, reduces vert transmit; cx lamivudine, myelosuppressives
- Emtricitabine: HIV+hepB; fluorinated lamivudine
- Lamivudine: HIV1+hepB (potent); pancreatitis and high resistance risk
- Didanosine: pancreatic tox, blindness; cx delavirdine, indinavir, atazanavir
- Abacavir: general NRTI
- Stavudine: cx advanced immunosuppression
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3 NNRTIs
- Delavirdine: skin rash and Stevens-Johnson; cx pregnancy
- Efavirenz: depression, mania, psychosis; cx pregnancy
- Nevirapine: Stevens-Johnson, fulminant hepatitis; single dose vert transmit protection
- binds HIV1 reverse transcriptase, inhibiting viral DNA pols
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5 antiretroviral PIs
- Atazanavir: no Cushings; Cx indinavir (CYP3A4 inhibitor)
- Indinavir: CYP3A4 inhibitor
- Lopinavir: combos with ritonavir
- Ritonavir: potent CYP3A4 inhibitor, combos with other PIs for lower effective dose
- Saquinavir: Cx delavirdine
- all of the above are also Cx with same as NNRTIs
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1 antiretroviral Integrase Inhibitor
Raltegravir: binds integrase; Tx-experienced, multi-drug resistant HIV1
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2 antiretroviral Entry Inhibitors
- Enfuvirtide: binds gp41, preventing conf. change required for fusion to cell (f = 41)
- Maraviroc: binds host CCR5, preventing viral adhesion (specific to R5 strain)
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